stf-118804

Description: STF-118804 is a highly specific and potent inhibitor of NAMPT (nicotinamide phosphoribosyl transferase) with IC50 values in the low nanomolar range. STF-118804 reduces the viability of B-ALL cell lines containing MLL chromosomal translations. In addition, leukemic samples from ?ve pediatric ALL patients are also sensitive to STF-118804 in the low nanomolar range. STF-118804 induces leukemia MV411 cell apoptosis without antecedent cell cycle arrest. STF-118804 improves survival in an orthotopic xenotransplant model of high-risk acute lymphoblastic leukemia, and targets leukemia stem cells. STF-118804 was also tolerated well in the efficacious dose range, and the absence of adverse physical or pathological effects indicated that toxicity was not limiting in a 20-day study of mock transplanted mice.

References: Chem Biol. 2013 Nov 21; 20(11):1352-63.